| Literature DB >> 19138519 |
Jinming Zhou1, Guoyan Geng, Gerald Batist, Jian Hui Wu.
Abstract
We report the SAR studies of 43 ionone-based chalcones that demonstrate substantial in vitro anti-proliferative activities in LNCaP, MDA-PCa-2b, 22Rv1, C4-2B and PC-3 prostate cancer cell lines. Compound 25 with an IC(50) value of 0.74 microM in LNCaP cells potently antagonizes DHT-induced transactivation of the wild type and the clinically relevant T877A, W741C and H874Y mutated androgen receptors, representing a novel chalcone as pan-antagonist of androgen receptor.Entities:
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Year: 2008 PMID: 19138519 DOI: 10.1016/j.bmcl.2008.12.089
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823